JP5496899B2 - シチジンデアミナーゼ阻害剤としての2’−フルオロ−2’−デオキシテトラヒドロウリジン - Google Patents
シチジンデアミナーゼ阻害剤としての2’−フルオロ−2’−デオキシテトラヒドロウリジン Download PDFInfo
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- JP5496899B2 JP5496899B2 JP2010530110A JP2010530110A JP5496899B2 JP 5496899 B2 JP5496899 B2 JP 5496899B2 JP 2010530110 A JP2010530110 A JP 2010530110A JP 2010530110 A JP2010530110 A JP 2010530110A JP 5496899 B2 JP5496899 B2 JP 5496899B2
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- compound
- cancer
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- 0 *[C@](C(N(CCC(N1)O)C1=O)O[C@]1CO)[C@]1O Chemical compound *[C@](C(N(CCC(N1)O)C1=O)O[C@]1CO)[C@]1O 0.000 description 2
- YYKPWSPWWHZLTO-JPCDQAEASA-N CC([C@@H]1F)O[C@H](CO)[C@H]1O Chemical compound CC([C@@H]1F)O[C@H](CO)[C@H]1O YYKPWSPWWHZLTO-JPCDQAEASA-N 0.000 description 1
- OIVLITBTBDPEFK-UHFFFAOYSA-N O=C(CCN1)NC1=O Chemical compound O=C(CCN1)NC1=O OIVLITBTBDPEFK-UHFFFAOYSA-N 0.000 description 1
- XOQSIJJEPLQOPY-KDBQFOGNSA-N OC(C1)C1([C@H]1O)OC(CN(CC[C@@H](N2)O)C2=O)[C@@H]1F Chemical compound OC(C1)C1([C@H]1O)OC(CN(CC[C@@H](N2)O)C2=O)[C@@H]1F XOQSIJJEPLQOPY-KDBQFOGNSA-N 0.000 description 1
- DINLEAHFNSLTEA-XDTPYFJJSA-N OC[C@H]([C@H]([C@H]1F)O)OC1N(CCCN1)C1=O Chemical compound OC[C@H]([C@H]([C@H]1F)O)OC1N(CCCN1)C1=O DINLEAHFNSLTEA-XDTPYFJJSA-N 0.000 description 1
- RTGAEUWOUHUIHP-FMDGEEDCSA-N OC[C@H]([C@H]([C@H]1F)O)O[C@H]1N(CC[C@H](N1)O)C1=O Chemical compound OC[C@H]([C@H]([C@H]1F)O)O[C@H]1N(CC[C@H](N1)O)C1=O RTGAEUWOUHUIHP-FMDGEEDCSA-N 0.000 description 1
- BUUQDDOATLEQQW-XVKVHKPRSA-N O[C@@H]([C@H]1O)[C@@H](C=O)O[C@H]1N(CCC(N1)O)C1=O Chemical compound O[C@@H]([C@H]1O)[C@@H](C=O)O[C@H]1N(CCC(N1)O)C1=O BUUQDDOATLEQQW-XVKVHKPRSA-N 0.000 description 1
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H1/00—Processes for the preparation of sugar derivatives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
- C07H19/073—Pyrimidine radicals with 2-deoxyribosyl as the saccharide radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US98039707P | 2007-10-16 | 2007-10-16 | |
| US60/980,397 | 2007-10-16 | ||
| PCT/US2008/080163 WO2009052287A1 (en) | 2007-10-16 | 2008-10-16 | 2 ' -flu0r0-2 ' -deoxytetrahydrouridines as cytidine deaminase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014043175A Division JP5859588B2 (ja) | 2007-10-16 | 2014-03-05 | シチジンデアミナーゼ阻害剤としての2’−フルオロ−2’−デオキシテトラヒドロウリジン |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011500713A JP2011500713A (ja) | 2011-01-06 |
| JP2011500713A5 JP2011500713A5 (enExample) | 2011-12-01 |
| JP5496899B2 true JP5496899B2 (ja) | 2014-05-21 |
Family
ID=40251685
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010530110A Active JP5496899B2 (ja) | 2007-10-16 | 2008-10-16 | シチジンデアミナーゼ阻害剤としての2’−フルオロ−2’−デオキシテトラヒドロウリジン |
| JP2014043175A Active JP5859588B2 (ja) | 2007-10-16 | 2014-03-05 | シチジンデアミナーゼ阻害剤としての2’−フルオロ−2’−デオキシテトラヒドロウリジン |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014043175A Active JP5859588B2 (ja) | 2007-10-16 | 2014-03-05 | シチジンデアミナーゼ阻害剤としての2’−フルオロ−2’−デオキシテトラヒドロウリジン |
Country Status (39)
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2012522842A (ja) * | 2009-04-06 | 2012-09-27 | エーザイ インコーポレイテッド | シチジンベースの抗新生物薬とシチジンデアミナーゼ阻害薬との組合せ、および癌の治療におけるその使用 |
| JP2014177455A (ja) * | 2007-10-16 | 2014-09-25 | Eisai Inc | シチジンデアミナーゼ阻害剤としての2’−フルオロ−2’−デオキシテトラヒドロウリジン |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US8404716B2 (en) | 2002-10-15 | 2013-03-26 | Celgene Corporation | Methods of treating myelodysplastic syndromes with a combination therapy using lenalidomide and azacitidine |
| US11116782B2 (en) | 2002-10-15 | 2021-09-14 | Celgene Corporation | Methods of treating myelodysplastic syndromes with a combination therapy using lenalidomide and azacitidine |
| US7964580B2 (en) | 2007-03-30 | 2011-06-21 | Pharmasset, Inc. | Nucleoside phosphoramidate prodrugs |
| NZ623495A (en) | 2008-05-15 | 2015-08-28 | Celgene Corp | Oral formulations of cytidine analogs and methods of use thereof |
| US8173621B2 (en) | 2008-06-11 | 2012-05-08 | Gilead Pharmasset Llc | Nucleoside cyclicphosphates |
| US20100055047A1 (en) * | 2008-08-26 | 2010-03-04 | Yiyu Zou | Methods for treating bronchial premalignancy and lung cancer |
| NZ593647A (en) | 2008-12-23 | 2013-08-30 | Gilead Pharmasset Llc | Synthesis of purine nucleosides |
| JO3262B1 (ar) * | 2009-04-06 | 2018-09-16 | Otsuka Pharma Co Ltd | توليفة من ديسيتابين مع مثبط سيتيدين دي أميناز واستخدامها في علاج السرطان |
| US8609631B2 (en) | 2009-04-06 | 2013-12-17 | Eisai Inc. | Compositions and methods for treating cancer |
| WO2010118006A1 (en) | 2009-04-06 | 2010-10-14 | Eisai Inc. | (2 ' -deoxy-ribofuranosyl) -1,3,4, 7-tetrahydro- (1,3) iazepin-2-0ne derivatives for treating cancer |
| GB0907551D0 (en) | 2009-05-01 | 2009-06-10 | Univ Dundee | Treatment or prophylaxis of proliferative conditions |
| TWI576352B (zh) | 2009-05-20 | 2017-04-01 | 基利法瑪席特有限責任公司 | 核苷磷醯胺 |
| US8618076B2 (en) | 2009-05-20 | 2013-12-31 | Gilead Pharmasset Llc | Nucleoside phosphoramidates |
| JP2013527145A (ja) | 2010-03-31 | 2013-06-27 | ギリード・ファーマセット・エルエルシー | リン含有活性化剤の立体選択的合成 |
| PL3290428T3 (pl) | 2010-03-31 | 2022-02-07 | Gilead Pharmasset Llc | Tabletka zawierająca krystaliczny (S)-2-(((S)-(((2R,3R,4R,5R)-5-(2,4-diokso-3,4-dihydropirymidyn-1(2H)-ylo)-4-fluoro-3-hydroksy-4-metylotetrahydrofuran-2-ylo)metoksy)(fenoksy)fosforylo)amino)propanian izopropylu |
| JP6069215B2 (ja) | 2010-11-30 | 2017-02-01 | ギリアド ファーマセット エルエルシー | 化合物 |
| DE202012013382U1 (de) | 2011-09-16 | 2016-08-23 | Gilead Pharmasset Llc | Zusammensetzungen zur Behandlung von HCV |
| US8889159B2 (en) | 2011-11-29 | 2014-11-18 | Gilead Pharmasset Llc | Compositions and methods for treating hepatitis C virus |
| EP3650013A1 (en) | 2013-01-31 | 2020-05-13 | Gilead Pharmasset LLC | Combination formulation of two antiviral compounds |
| EA201690473A1 (ru) | 2013-08-27 | 2017-03-31 | ГАЙЛИД ФАРМАССЕТ ЭлЭлСи | Комбинированный состав двух противовирусных соединений |
| KR102272773B1 (ko) * | 2013-10-29 | 2021-07-02 | 오츠카 세이야쿠 가부시키가이샤 | 2'-데옥시-2',2'-디플루오로테트라하이드로우리딘의 합성 경로 |
| MX385778B (es) | 2014-04-04 | 2025-03-18 | Del Mar Pharmaceuticals | Uso de dianhidrogalactitol y análogos o derivados del mismo para tratar cáncer de células no pequeñas del pulmón y cáncer de ovario. |
| KR20170042598A (ko) | 2014-08-22 | 2017-04-19 | 셀진 코포레이션 | 항체와 조합된 면역조절 화합물을 이용하여 다발성 골수종을 치료하는 방법 |
| MX393043B (es) * | 2015-12-03 | 2025-03-24 | Epidestiny Inc | Composiciones que contienen decitabina, 5azacitidina y tetrahidrouridina y sus usos |
| WO2017158396A1 (en) * | 2016-03-16 | 2017-09-21 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Cytidine deaminase inhibitors for the treatment of pancreatic cancer |
| KR20200118827A (ko) | 2018-02-02 | 2020-10-16 | 마베릭스 온콜로지, 잉크. | 젬시타빈 모노포스페이트의 소분자 약물 컨쥬게이트 |
| EP3844477A4 (en) * | 2018-08-28 | 2023-01-04 | Essenlix Corporation | IMPROVING THE ACCURACY OF A DOSAGE |
| US11224610B2 (en) * | 2018-09-19 | 2022-01-18 | Otsuka Pharmaceutical Co., Ltd. | Low dose combination CDA substrate drug/cedazuridine with extended administration |
| US12448624B2 (en) | 2018-10-19 | 2025-10-21 | Interoligo Corporation | Modified nucleic acid having improved treatment efficacy, and anticancer pharmaceutical composition containing same |
| KR102280330B1 (ko) * | 2018-10-19 | 2021-07-21 | 인터올리고 주식회사 | 치료 효능을 개선한 핵산 변형체 및 이를 포함하는 항암용 약학 조성물 |
| BR112022006523A2 (pt) * | 2019-10-08 | 2022-06-28 | Otsuka Pharma Co Ltd | 2'-desóxi-2',2'-difluorotetraidrouridinas com alta pureza e métodos para produção da mesma |
| PH12022552250A1 (en) * | 2020-02-25 | 2023-11-13 | Otsuka Pharma Co Ltd | Combination decitabine and cedazuridine solid oral dosage forms |
| EP4313069A4 (en) * | 2021-03-26 | 2024-12-18 | The Cleveland Clinic Foundation | TREATMENT OF RNA VIRUS INFECTION WITH A CYTIDINE INDEAMINASE INHIBITOR |
| WO2022254457A1 (en) * | 2021-05-29 | 2022-12-08 | Msn Laboratories Private Limited, R&D Center | An improved process for the preparation of (4r)-1-[(2r,4r,5r)-3,3-difluoro-4-hydroxy-5-(hydroxymethyl) oxolan-2-yl]-4-hydroxy-1,3-diazinan-2one and its intermediate compounds |
| JP2024539267A (ja) | 2021-10-19 | 2024-10-28 | アキラバイオ, インコーポレイテッド | 2’-デオキシシチジンアナログを含む組成物、ならびに鎌状赤血球症、サラセミアおよびがんを処置するためのその使用 |
| WO2023076332A1 (en) * | 2021-11-01 | 2023-05-04 | St. John's University | Injectable liquid pharmaceutical compostion containing gemcitabine and a cytidine deaminase inhibitor |
| US20230271996A1 (en) * | 2021-12-25 | 2023-08-31 | Scinopharm Taiwan, Ltd. | Process for preparing cedazuridine |
| EP4580635A1 (en) | 2022-08-31 | 2025-07-09 | Taiho Pharmaceutical Co., Ltd. | Combination therapies for treatment of t-cell lymphomas with tolinapant, cedazuridine and decitabine |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| JP2014177455A (ja) * | 2007-10-16 | 2014-09-25 | Eisai Inc | シチジンデアミナーゼ阻害剤としての2’−フルオロ−2’−デオキシテトラヒドロウリジン |
| JP2012522842A (ja) * | 2009-04-06 | 2012-09-27 | エーザイ インコーポレイテッド | シチジンベースの抗新生物薬とシチジンデアミナーゼ阻害薬との組合せ、および癌の治療におけるその使用 |
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